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帕金森病患者使用阿扑吗啡的情况。

Apomorphine in patients with Parkinson's disease.

作者信息

Muguet D, Broussolle E, Chazot G

机构信息

Service de Neurologie C, Hôpital Neurologique et Neurochirurgical Pierre Wertheimer, Lyon, France.

出版信息

Biomed Pharmacother. 1995;49(4):197-209. doi: 10.1016/0753-3322(96)82620-5.

Abstract

We present a review of the recent literature and personal experience with apomorphine in patients with Parkinson's disease. Apomorphine is a potent D1 and D2 dopaminergic agonist. It has a rapid and short duration effect after subcutaneous administration at doses ranging from 15 to 180 micrograms/kg. Plasma maximal concentration is reached in 8-16 minutes, with a plasma half life of 34-70 minutes. Bioavailability is close to 100%. Repeated injections in patients show post-stimulative hyposensitivity. Apomorphine test appears very useful for the differential diagnosis between idiopathic Parkinson's disease and other Parkinson plus syndromes, and as a predictive test for dopaminergic responsiveness. Appropriate doses are able to alleviate akinesia, rigidity and tremor. Recent therapeutic trials have demonstrated the high interest of intermittent multiple subcutaneous apomorphine injections to cut the "off" motor phases in fluctuating parkinsonian patients under chronic levodopa treatment. In some cases, continuous apomorphine subcutaneous infusion with a portable pump may be required, particularly when levodopa treatment is temporarily interrupted, as after abdominal surgery. During long-term treatment, the apomorphine dose able to relieve akinesia remains stable. Peripheral side effects such as nausea and hypotension may be prevented by the co-administration of domperidone, a peripheral dopaminergic antagonist. Cutaneous fibrous nodules and psychiatric symptoms may occur, but usually at high dosages with continuous infusion. Local allergic effects have limited the use of other routes of administration, such as intranasal, sublingual, and rectal routes. Apomorphine is also used as a pharmacological tool for clinical research with the aim of a better understanding of the pathophysiology of Parkinson's disease.

摘要

我们对近期有关帕金森病患者使用阿扑吗啡的文献及个人经验进行综述。阿扑吗啡是一种强效的D1和D2多巴胺能激动剂。皮下注射剂量为15至180微克/千克时,起效迅速且作用持续时间短。8至16分钟达到血浆最大浓度,血浆半衰期为34至70分钟。生物利用度接近100%。对患者重复注射会出现刺激后低敏现象。阿扑吗啡试验对特发性帕金森病与其他帕金森叠加综合征的鉴别诊断似乎非常有用,并且可作为多巴胺能反应性的预测试验。适当剂量能够缓解运动不能、僵硬和震颤。近期的治疗试验表明,间歇性多次皮下注射阿扑吗啡对于减轻慢性左旋多巴治疗的波动性帕金森病患者的“关”期运动症状具有很高的价值。在某些情况下,可能需要使用便携式泵进行阿扑吗啡皮下持续输注,尤其是在左旋多巴治疗暂时中断时,如腹部手术后。在长期治疗过程中,能够缓解运动不能的阿扑吗啡剂量保持稳定。外周多巴胺能拮抗剂多潘立酮的联合使用可预防恶心和低血压等外周副作用。皮肤纤维结节和精神症状可能会出现,但通常在高剂量持续输注时发生。局部过敏反应限制了鼻内、舌下和直肠等其他给药途径的使用。阿扑吗啡还用作临床研究的药理学工具,目的是更好地理解帕金森病的病理生理学。

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